FLT3 RECEPTOR ANTAGONISTS Russian patent published in 2020 - IPC C07D233/64 C07D295/26 C07D401/12 C07D235/18 C07D403/04 C07D263/57 C07D249/08 C07D209/08 C07D413/04 C07D413/12 A61K31/506 A61K31/5377 A61K31/4523 A61K31/4453 A61K31/496 A61K31/423 A61K31/4178 A61K31/415 A61K31/4196 A61P35/00 

Abstract RU 2710928 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (2) and variants thereof, which are FLT3 receptor antagonists. In general structural formula (2)

X is CONH or triazolyl; Y is SO2, Q is selected from a group of formulas:

and ,

where Q1 and Q2 are CH; Q3 is selected from O, S, N and NH; Q4 is selected from C, N and CO; Q5 is selected from C and N; R6 is selected from H, OH, alkyl, hydroxyalkyl and alkoxy, R1 is OH; R2 is H; R3 is selected from H, OR11, halogen and O-(CH2)p-O-alkyl; R4 is selected from H, alkyl, halogen, CN, trifluoromethyl, CO-alkyl, phenyl and benzyl; provided that one of R3 and R4 is H; R5 is H; two of R2 and R3, or R3 and R4, or R4 and R5 together with carbon atoms, to which they are bonded, form an aromatic ring containing 5–6 members, and the rest of R2-R5 are H, R7 and R8 are alkyl or R7 and R8 together with atom N, to which they are attached, form group of formulas:

, or ,

where R10 is selected from H, alkyl, halogen, trifluoromethyl, aryl and hydroxyalkyl, or two adjacent groups R10 together with ring atoms, to which they are bonded, form an aryl group; or R7 and R8 together with atom N, to which they are attached form group of formula , where Z is a group NR14, where R14 is selected from phenyl, benzyl and pyrimidyl, or R7 is H and R8 is cycloalkyl, preferably cyclohexyl and adamantyl, R11 is H or alkyl; R15 represents a group selected from H, halogen, OH and alkoxy; s is 0, 1, 2 or 3; n is 1 with the exception of N-(5-chloro-2-hydroxyphenyl)-3-(piperidin-1-sulphonyl) benzamide. Invention also relates to versions of the compound of formula (2) - compounds (1), (2a), (2b), (2c) and (2d) and to a group of specific compounds which are described in the patent claim.

EFFECT: inventions can be used for treating pain disorders, pain disorders are selected from neuropathic pain, iatrogenic pain, including cancer pain, infectious pain, including herpetic pain, central pain, nociceptive pain, including postoperative pain, and back pain and orofacial area.

13 cl, 1 tbl, 13 ex

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RU 2 710 928 C2

Authors

Valme Zhan

Leri Zhan-Filipp

Ronyan Dide

Shmitt Martin

Dates

2020-01-14Published

2015-07-30Filed